Topical penetration of commercial salicylate esters and salts using human isolated skin and clinical microdialysis studies.

@article{Cross1998TopicalPO,
  title={Topical penetration of commercial salicylate esters and salts using human isolated skin and clinical microdialysis studies.},
  author={Sheree E. Cross and Chris Anderson and Michael S. Roberts},
  journal={British journal of clinical pharmacology},
  year={1998},
  volume={46 1},
  pages={
          29-35
        }
}
AIMS The penetration of active ingredients from topically applied anti-inflammatory pharmaceutical products into tissues below the skin is the basis of their therapeutic efficacy. There is still controversy as to whether these agents are capable of direct penetration by diffusion through the tissues or whether redistribution in the systemic circulation is responsible for their tissue deposition below the application site. METHODS The extent of direct penetration of salicylate from commercial… Expand
Percutaneous absorption of topically applied NSAIDS and other compounds: Role of solute properties, skin physiology and delivery systems
TLDR
The pharmacokinetics of NSAIDs in the dermis and other tissues appears to be related to the absorption of solutes through the stratum corneum, binding of the NSAIDs to dermal andother tissues and clearance of NSAID from these tissues through either diffusion into deeper tissues or removal by the systemic blood supply. Expand
Self Promotion of Deep Tissue Penetration and Distribution of Methylsalicylate After Topical Application
TLDR
In vivo tissue and plasma concentrations of salicylate in rats rose rapidly in the first 1 hr and were more than the predicted 1.4-fold higher for MeSA, mirrored by the increase in blood flow induced by MeSA in human cutaneous vessels and that reported in the literature. Expand
Differentiated in vivo skin penetration of salicylic compounds in hairless rats measured by cutaneous microdialysis.
TLDR
Investigation of in vivo skin penetration of four 14C-salicylic compounds using microdialysis and to relate dermal concentrations to structural features found differentiated penetration kinetics was found, finding protein binding and dissociation may explain the lowerdermal concentrations of 14 C- salicylic acid and 14D-diethylamine salicylate. Expand
Convective transport of highly plasma protein bound drugs facilitates direct penetration into deep tissues after topical application.
TLDR
A physiologically based pharmacokinetic model was applied to interpret published human microdialysis data, estimated in vitro dermal diffusion and protein binding affinity of drugs that have been previously applied topically in vivo and measured in deep cutaneous tissues over time and found convective blood, lymphatic and interstitial flow led to significant deep tissue concentrations for drugs that are highly plasma protein bound. Expand
Regional differences in the in vitro penetration of methylsalicylate through equine skin.
TLDR
It was concluded that the commercial formulation of MeSa would achieve therapeutic levels of total salicylate beneath sites of topical application, with a faster and more pronounced response through the leg region, compared to the upper body. Expand
Modelling of drug permeation in human skin in vitro from finite dose applications
TLDR
A new physiological pharmacokinetic model to describe the effect of blood flow, blood protein binding and dermal binding on the rate and depth of penetration of topical drugs into the underlying skin shows that dermal diffusion alone cannot explain the in vivo data and blood and/or lymphatic transport to deep tissues must be present for almost all of the drugs tested. Expand
Bioequivalence of topical formulations in humans: evaluation by dermal microdialysis sampling and the dermatopharmacokinetic method.
TLDR
DMD sampling proved effective and variability analyses demonstrated the feasibility of BE studies in as little as 18 subjects, with 3- to 5-fold higher lidocaine penetration from cream formulation than from ointment. Expand
Penetration of a topically applied nonsteroidal anti-inflammatory drug into local tissues and synovial fluid of dogs.
TLDR
Topically applied NSAIDs can penetrate deeply into tissues and synovial fluid and local concentrations higher than circulating systemic concentrations are suggestive that direct diffusion and local blood redistribution are contributing to this effect. Expand
Modeling the human skin barrier--towards a better understanding of dermal absorption.
TLDR
The understanding of skin physiology and the experimentally observed mechanisms of transdermal drug transport inform the current models of drug penetration and distribution in the skin, reflecting the most recent directions of investigation. Expand
Critical evaluation and methodological positioning of the transdermal microdialysis technique. A review.
TLDR
Transdermal microdialysis technique is a traditional in vivo method for investigating the alterations of the biochemical milieu in the skin and is an important element of the toolbox of preclinical and clinical dermal pharmacokinetic/pharmacodynamic assays. Expand
...
1
2
3
4
5
...

References

SHOWING 1-10 OF 33 REFERENCES
Skin permeability and local tissue concentrations of nonsteroidal anti-inflammatory drugs after topical application.
  • P. Singh, M. Roberts
  • Chemistry, Medicine
  • The Journal of pharmacology and experimental therapeutics
  • 1994
TLDR
The predicted tissue concentrations of each NSAID after its application to human epidermis was made by a convolution of the epidermal and underlying tissue concentration-time profiles, and the estimated tissue concentrations could be related to their maximal fluxes across epidersmis from an applied vehicle. Expand
Effects of vasoconstriction on dermal pharmacokinetics and local tissue distribution of compounds.
TLDR
Phenylephrine can significantly increase quantities of solutes delivered to local tissues after dermal application, the observed effects being due to the vasoconstrictive properties of phenylephrine. Expand
Local deep tissue penetration of compounds after dermal application: structure-tissue penetration relationships.
  • P. Singh, M. Roberts
  • Chemistry, Medicine
  • The Journal of pharmacology and experimental therapeutics
  • 1996
TLDR
Deep tissue penetration of solutes after application, as aqueous solutions, to the epidermis is greater for smaller solutes with adequate lipophilicity, based on the preliminary qualitative and quantitative analysis. Expand
Microdialysis in cutaneous pharmacology: kinetic analysis of transdermally delivered nicotine.
TLDR
Microdialysis may be a novel, powerful tool to study cutaneous pharmacology in vivo, and nicotine kinetics were independent of skin barrier function, as assessed by transepidermal water loss. Expand
The effect of protein binding on the deep tissue penetration and efflux of dermally applied salicylic acid, lidocaine and diazepam in the perfused rat hindlimb.
TLDR
It is shown that protein binding significantly affects the deep tissue penetration and distribution of dermally applied solutes and that this effect is more prominent for highly protein-bound solutes. Expand
Serum Concentrations of Salicylic Acid following Topically Applied Salicylate Derivatives
TLDR
A considerable amount of salicylic acid may be absorbed through the skin after topical application of methyl salicylate products and this may increase with multiple applications, so caution is warranted in patients for whom systemic saliylate may be hazardous or problematic. Expand
In vivo characterization of transdermal drug transport by microdialysis
Abstract The aim of the present study was to evaluate the scope and limitations of the microdialysis technique as a tool for pharmacokinetic studies of transdermal therapy systems (TTS) and forExpand
Effect of Perfusion Flow Rate on the Tissue Uptake of Solutes After Dermal Application Using the Rat Isolated Perfused Hindlimb Preparation
TLDR
It is concluded that the rat perfused hindlimb preparation successfully combines many of the advantages of in‐vitro and in-vivo methods and has potential for routine use in the study of solute dermal absorption kinetics. Expand
Ethanol absorption across human skin measured by in vivo microdialysis technique.
TLDR
This initial study investigates the technique's usefulness in the field of percutaneous absorption of solvents, using ethanol as test substance, and opens new possibilities in the investigation of skin barrier function in man. Expand
Kinetics of transdermal penetration of an organic ion pair: physostigmine salicylate.
TLDR
It is proposed that the apparent volume of distribution of physostigmine is larger than that of salicylate and, hence, a smaller concentration difference across the diffusion barrier exists for physostIGmine, which can explain the lower flux of physstigmine to conform to Fick's first law of diffusion and the assumption of equal molar transfer to the skin of both species. Expand
...
1
2
3
4
...